Abstract
The SAR of 2-pyridyl-3,5-diaryl pyrroles, ligands of the human glucagon receptor and inhibitors of p38 kinase, were investigated. This effort resulted in the identification of 2-(4-pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)pyrr ole 49 (L-168,049), a potent (Kb = 25 nM), selective antagonist of glucagon.
MeSH terms
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Animals
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Calcium-Calmodulin-Dependent Protein Kinases / antagonists & inhibitors*
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Humans
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Mice
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Mitogen-Activated Protein Kinases*
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Pyridines / chemical synthesis
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Pyridines / chemistry
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Pyridines / pharmacology*
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Pyrroles / chemical synthesis
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Pyrroles / chemistry
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Pyrroles / pharmacology*
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Receptors, Glucagon / antagonists & inhibitors*
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Structure-Activity Relationship
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p38 Mitogen-Activated Protein Kinases
Substances
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Enzyme Inhibitors
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L 168049
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Pyridines
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Pyrroles
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Receptors, Glucagon
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Calcium-Calmodulin-Dependent Protein Kinases
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Mitogen-Activated Protein Kinases
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p38 Mitogen-Activated Protein Kinases